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Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists.
Tseng SL, Hung MS, Chang CP, Song JS, Tai CL, Chiu HH, Hsieh WP, Lin Y, Chung WL, Kuo CW, Wu CH, Chu CM, Tung YS, Chao YS, Shia KS. Tseng SL, et al. J Med Chem. 2008 Sep 11;51(17):5397-412. doi: 10.1021/jm800066v. Epub 2008 Aug 20. J Med Chem. 2008. PMID: 18712856
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice.
Wu CH, Hung MS, Song JS, Yeh TK, Chou MC, Chu CM, Jan JJ, Hsieh MT, Tseng SL, Chang CP, Hsieh WP, Lin Y, Yeh YN, Chung WL, Kuo CW, Lin CY, Shy HS, Chao YS, Shia KS. Wu CH, et al. Among authors: tseng sl. J Med Chem. 2009 Jul 23;52(14):4496-510. doi: 10.1021/jm900471u. J Med Chem. 2009. PMID: 19530697
Discovery of 1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice.
Chang CP, Wu CH, Song JS, Chou MC, Wong YC, Lin Y, Yeh TK, Sadani AA, Ou MH, Chen KH, Chen PH, Kuo PC, Tseng CT, Chang KH, Tseng SL, Chao YS, Hung MS, Shia KS. Chang CP, et al. Among authors: tseng sl, tseng ct. J Med Chem. 2013 Dec 27;56(24):9920-33. doi: 10.1021/jm401158e. Epub 2013 Dec 4. J Med Chem. 2013. PMID: 24224693
29 results